C=o Bonded Directly To The Six-membered Hetero Ring Patents (Class 514/350)
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Patent number: 8618305Abstract: The present invention provides dimethyl sulphoxide solvate of 4-(4-{3-[4-chloro-3 -(trifluoromethyl)phenyl]ureido}phenoxy)-N2-methylpyridine-2-carboxamide, process for its preparation, pharmaceutical composition comprising it and its use for the treatment of cancer. The present invention also provides a novel HPLC method for the identification, quantification and isolation of related substances of sorafenib.Type: GrantFiled: January 28, 2011Date of Patent: December 31, 2013Assignee: Ranbaxy Laboratories LimitedInventors: Jagdev Singh Jaryal, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad, Sachin Deorao Zade, Ajay Shankar Singh
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Patent number: 8614329Abstract: The present invention provides amorphous and crystalline forms of acid addition salts of sorafenib, pharmaceutical compositions comprising them, and their use for the treatment of cancer. The present invention also provides processes for the preparation of acid addition salts of sorafenib.Type: GrantFiled: June 7, 2013Date of Patent: December 24, 2013Assignee: Ranbaxy Laboratories LimitedInventors: Jagdev Singh Jaryal, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
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Publication number: 20130338198Abstract: A skin disorder treatment composition and method for treating a skin disorder or symptoms of a skin disorder are provided. The composition includes: about 0.0001 wt. % to about 5 wt. % of a serine protease inhibitor; about 2 wt. % to about 10 wt. % of a hydrophobic polymer/hydrophilic polymer complex comprising a poly(vinylpyrrolidone-alkylene) polymer wherein the alkylene group contains at least 10 carbon atoms and a cellulose containing polymer; about 0.5 wt. % to about 20 wt. % of a release agent; and at least about 50 wt. % water. The skin disorder or the symptom of skin disorder from ichthyosis, dermatitis, eczema, rosacea, psoriasis, inflammation, xerosis, or urticaria.Type: ApplicationFiled: December 9, 2011Publication date: December 19, 2013Applicant: Skinvisible Pharmaceuticals, Inc.Inventor: James A. Roszell
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Patent number: 8609701Abstract: Methods are provided for administering pirfenidone to a patient that has exhibited abnormal biomarkers of liver function in response to pirfenidone administration. The methods include administering to a patient pirfenidone at doses lower than the full target dosage for a time period, followed by administering to the patient pirfenidone at the full target dosage. The methods also include administering pirfenidone at the full target dose with no reduction and administering permanently reduced doses of pirfenidone.Type: GrantFiled: November 9, 2009Date of Patent: December 17, 2013Assignee: Intermune, Inc.Inventors: Williamson Ziegler Bradford, Javier Szwarcberg
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Patent number: 8604208Abstract: The present invention provides amorphous and crystalline forms of acid addition salts of sorafenib, pharmaceutical compositions comprising them and their use for the treatment of cancer. The present invention also provides processes for the preparation of acid addition salts of sorafenib.Type: GrantFiled: September 24, 2010Date of Patent: December 10, 2013Assignee: Ranbaxy Laboratories LimitedInventors: Jagdev Singh Jaryal, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
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Patent number: 8598210Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: GrantFiled: November 20, 2012Date of Patent: December 3, 2013Assignee: Akebia Therapeutics, Inc.Inventors: Richard Masaru Kawamoto, Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer
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Publication number: 20130317001Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.Type: ApplicationFiled: May 21, 2013Publication date: November 28, 2013Applicants: XENON PHARMACEUTICALS INC., GENENTECH, INC.Inventors: Jean-Christophe Andrez, Sultan Chowdhury, Shannon Marie Decker, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Jun Li, Daniel F. Ortwine, Brian Safina, Tao Sheng, Shaoyi Sun, Daniel P. Sutherlin, Michael Scott Wilson, Alla Yurevna Zenova
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Publication number: 20130317000Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.Type: ApplicationFiled: May 21, 2013Publication date: November 28, 2013Applicants: XENON PHARMACEUTICALS INC., GENENTECH, INCInventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
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Patent number: 8592462Abstract: Methods are provided for administering pirfenidone to a patient that has exhibited abnormal biomarkers of liver function in response to pirfenidone administration. The methods include administering to a patient pirfenidone at doses lower than the full target dosage for a time period, followed by administering to the patient pirfenidone at the full target dosage. The methods also include administering pirfenidone at the full target dose with no reduction and administering permanently reduced doses of pirfenidone.Type: GrantFiled: December 6, 2011Date of Patent: November 26, 2013Assignee: Intermune, Inc.Inventors: Williamson Ziegler Bradford, Javier Szwarcberg
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Publication number: 20130303548Abstract: Niacin prevents and/or reverses the development of experimental hepatic steatosis, deposition of triglycerides in liver and serum of individuals, deposition of total cholesterol in liver and serum in individuals, and inhibit liver lipid peroxidation and oxidative stress in individuals at risk of developing fatty liver disease or NAFLD. In cultured human hepatocytes, niacin inhibits alcohol-induced fat accumulation.Type: ApplicationFiled: November 22, 2011Publication date: November 14, 2013Applicant: The Regents of the University of CaliforniaInventors: Moti L. Kashyap, Shobha V. Kamanna, Vaijinath S. Kamanna
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Publication number: 20130296380Abstract: A compound of Formula (I), salts thereof, prodrugs thereof, metabolites thereof, pharmaceutical compositions containing such a compound, and use of such compound and compositions to treat diseases mediated by multiple kinases, such as raf, VEGFR, PDGFR, FLT-3, and c-Kit.Type: ApplicationFiled: January 5, 2012Publication date: November 7, 2013Applicant: Beta Pharma Canada Inc.Inventors: Zhaoyin Wang, Chunrong Yu
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Patent number: 8575202Abstract: Stabilized cationic ammonium compounds are described. The compounds are stabilized with pyridine-based chelators and/or heteroketo-based chelators that impede the generation of nitrogen comprising groups from the cationic ammonium compounds.Type: GrantFiled: November 6, 2012Date of Patent: November 5, 2013Assignee: Conopco, Inc.Inventors: Van Au, Stephen Alan Madison
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Patent number: 8569543Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: GrantFiled: August 30, 2011Date of Patent: October 29, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
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Patent number: 8552197Abstract: The present invention provides sorafenib ethane sulphonate, process for its preparation, pharmaceutical composition comprising sorafenib ethane sulphonate and its use for the treatment of cancer. Formula (III).Type: GrantFiled: November 12, 2010Date of Patent: October 8, 2013Assignee: Ranbaxy Laboratories LimitedInventors: Jagdev Singh Jaryal, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
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Publication number: 20130261120Abstract: The present invention relates to: *combinations of: component A: one or more omega-carboxyaryl-substituted diphenyl urea compounds of general formula (I), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B: one or more N-(2-arylamino) aryl sulfonamide compounds of general formula (II), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; and, optionally, component C: one or more further pharmaceutical agents; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; *use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and *a kit comprising such a combination.Type: ApplicationFiled: September 29, 2011Publication date: October 3, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Florian PĆ¼hler, Marion Hitchcock
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Publication number: 20130245075Abstract: The present invention relates to melanogenesis inhibition using an effective amount of piper longumine obtained from the roots of Piper longum.Type: ApplicationFiled: March 15, 2013Publication date: September 19, 2013Inventors: Muhammed Majeed, Kalyanam Nagabhushanam
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Publication number: 20130245076Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: ApplicationFiled: April 9, 2013Publication date: September 19, 2013Applicants: Akebia Therapeutics Inc., Aerpio Therapeutics Inc.Inventors: Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
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Publication number: 20130209546Abstract: The invention relates to combining targeted therapies with selected chemotherapeutics for the treatment of melanoma. The invention provides a method for inducing apoptosis in a melanoma tumor cell by reducing Akt3 activity. A method for inducing apoptosis in a melanoma tumor cell comprising contacting a melanoma tumor cell with an agent that reduces Akt3 activity to restore normal apoptotic sensitivity to a melanoma tumor cell, allowing a lower concentration of chemotherapeutic agents resulting in decreased toxicity to a patient. Also disclosed is a method for treating a melanoma comprising administering an agent that reduces Akt3 activity and an agent that reduces V599E B-Raf activity, thereby treating a melanoma tumor.Type: ApplicationFiled: January 25, 2013Publication date: August 15, 2013Applicant: THE PENN STATE RESEARCH FOUNDATIONInventor: THE PENN STATE RESEARCH FOUNDATION
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Publication number: 20130203757Abstract: The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed.Type: ApplicationFiled: November 16, 2012Publication date: August 8, 2013Applicants: THE GENERAL HOSPITAL CORPORATION, CANTHERA THERAPEUTICS INC.Inventors: Canthera Therapeutics Inc., The General Hospital Corporation
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Publication number: 20130203816Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: ApplicationFiled: November 20, 2012Publication date: August 8, 2013Applicant: Akebia Therapeutics Inc.Inventors: Richard Masaru Kawamoto, Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer
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Publication number: 20130197016Abstract: The use of vascular endothelial growth factor receptor 2 inhibitors or a pharmaceutically acceptable salt thereof for the treatment of ocular vascular disease is provided. Dosing regimes, including once weekly administration, of certain VEGF-R2 inhibitors are provided which deliver therapeutically effective concentrations of the VEGF-R2 compounds in ocular tissues for at least one week for the treatment of ocular vascular disease.Type: ApplicationFiled: October 25, 2011Publication date: August 1, 2013Inventors: Mitchell Brigell, Peter End, Vinayak Hosagrahara, Bruce D. Jaffee, Erik Meredith, Ronald Keith Newton, Stephen Poor, Yubin Qiu
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Patent number: 8492412Abstract: The invention relates to a gel composition containing pirfenidone, which is advantageous over other cutaneously administered pharmaceutical forms known in the prior art and which can be used in treatment for the restoration of tissues with fibrotic lesions and for the prevention of fibrotic lesions.Type: GrantFiled: August 14, 2008Date of Patent: July 23, 2013Assignee: Cell Therapy and Technology, S.A. De C.V.Inventors: JosĆ© AgustĆn Rogelio MagaƱa Castro, Laura VĆ”zquez Cervantes, Juan Socorro ArmendĆ”riz Borunda
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Publication number: 20130183268Abstract: The present invention relates to drug combinations and pharmaceutical compositions for treating hyperproliferative disorders such as cancer including non-small cell lung carcinoma, said drug combination comprising (1) a fluoro-substituted-diaryl urea of Formula (I), (2) at least one antifolate and optionally (3) at least one platinum complex antineoplastic nucleic acid binding agent, where any of these components can be present in the form of a pharmaceutically acceptable salt or other derivative thereof.Type: ApplicationFiled: July 19, 2011Publication date: July 18, 2013Applicant: BAYER HEALTHCARE LLCInventors: Olaf Christensen, Iris Kuss
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Publication number: 20130171268Abstract: The present invention relates to compositions and methods for prophylactic and/or therapeutic treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more compounds selected from the group consisting of epicatechin, an epicatechin derivative, catechin, a catechin derivative, nicorandil, and a nicorandil derivative in an amount effective to ameliorate mitochondrial toxicity caused by administration of a chemical, food, or drug.Type: ApplicationFiled: June 5, 2012Publication date: July 4, 2013Inventors: Francisco Villarreal, Alan Maisel, George Schreiner, Guillermo M. Ceballos Reyes, Pam Taub
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Patent number: 8476448Abstract: The present invention relates to a novel solid form of 4-[[(6-chloropyridin-3-yl)methyl](2,2-difluoroethyl)amino]furan-2(5H)-one, to processes for its preparation and to its use in agrochemical preparations.Type: GrantFiled: October 31, 2012Date of Patent: July 2, 2013Assignee: Bayer Cropscience AGInventors: Britta Olenik, Robert Velten, Peter Jeschke, Norbert Lui, Christian Funke, Wolfgang Wirth
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Patent number: 8470854Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4āP-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: April 12, 2012Date of Patent: June 25, 2013Assignee: Bristol-Meyers Squibb CompanyInventor: Donald J. P. Pinto
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Patent number: 8470858Abstract: The present invention comprises an agave syrup stored for at least eight weeks, having phytochemicals preferably selected from the group comprising flavonoids, polycosanols and sapogenins, which provide anticancerigen and antioxidant properties to the agave syrup. It is also described an extract of said agave syrup and a related method for its extraction and application for inhibiting the growth of cancer cells.Type: GrantFiled: September 9, 2008Date of Patent: June 25, 2013Inventors: Janet-Alejandra Gutierrez-Uribe, Sergio Serna-Saldivar
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Publication number: 20130158076Abstract: The present invention relates to methylene urea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.Type: ApplicationFiled: February 15, 2013Publication date: June 20, 2013Applicant: MERCK PATENT GMBHInventor: Merck Patent GmbH
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Patent number: 8450347Abstract: The invention relates to a method of controlling feelings of pain in infants or diseased or elderly persons using a complete nutrition or a nutritional supplement. The method comprises administering increased levels of folic acid, vitamin B6 and vitamin B12 or their functional equivalents.Type: GrantFiled: February 19, 2008Date of Patent: May 28, 2013Assignee: N.V. NutriciaInventors: Robert Johan Joseph Hageman, Jacob Geert Bindels
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Publication number: 20130130898Abstract: The present invention relates to compositions of fungicidally active compounds comprising at least one active compound I selected from 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (3?,4?,5?-trifluoro-biphenyl-2-yl)-amide (fluxapyroxade), bixafen, fluopyram, isopyrazam, sedaxane, penflufen and penthiopyrad and at least one further active component II as defined below.Type: ApplicationFiled: August 2, 2011Publication date: May 23, 2013Inventors: Markus Gewehr, Jochen Dietz, Egon Haden
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Publication number: 20130131122Abstract: A compound of Formula (I): salts thereof, prodrugs thereof, metabolites thereof, pharmaceutical compositions containing such a compound, and use of such compound and compositions to treat diseases mediated by raf, VEGFR, PDGFR, p38 and flt-3.Type: ApplicationFiled: November 5, 2012Publication date: May 23, 2013Applicant: BAYER HEALTHCARE LLCInventor: Bayer Healthcare LLC
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Patent number: 8445687Abstract: There is provided a process for preparing sorafenib or a salt thereof comprising the use of a compound of formula (A) wherein R? is selected from the group consisting of hydrogen, āC(O)OA, āC(O)CX3, āC(O)NH2, āC(O)āNHOH or There is also provided intermediate compounds of general formula (A), N-methyl-4-(4-ureidophenoxy)picolinamide, 4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenylcarbamate derivative and N-methyl-4-(4-(2,2,2-trihaloacetamido)phenoxy)picolinamide, processes for their preparation and their use in the preparation of sorafenib.Type: GrantFiled: September 10, 2008Date of Patent: May 21, 2013Assignee: Cipla LimitedInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Maruti Ghagare, Sandip Chikhalikar
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Patent number: 8420674Abstract: The invention relates to methods for decreasing adverse events associated with pirfenidone (5-methyl-1-phenyl-2-(1H)-pyridone) therapy. The invention discloses an optimized dose escalation scheme that results in the patient having increased tolerance to adverse events associated with the administration of pirfenidone. The invention also discloses a starter pack that may be used in conjunction with the dose escalation scheme.Type: GrantFiled: July 7, 2010Date of Patent: April 16, 2013Assignee: Intermune, Inc.Inventor: Williamson Z. Bradford
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Patent number: 8410082Abstract: This invention relates to novel diaryl urea compounds, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of multiple kinases.Type: GrantFiled: May 20, 2010Date of Patent: April 2, 2013Assignee: Concert Pharmaceuticals, Inc.Inventors: Julie F. Liu, Roger D. Tung, Scott L. Harbeson
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Publication number: 20130065876Abstract: The present invention relates to compounds of formula I, wherein R1 to R5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof. The present invention relates also to the manufacture of said compounds, pharmaceutical compositions containing them and methods for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 11, 2012Publication date: March 14, 2013Inventors: Uwe Grether, Paul Hebeisen, Peter Mohr, Fabienne Ricklin, Stephan Roever
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Patent number: 8389570Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: GrantFiled: August 12, 2011Date of Patent: March 5, 2013Assignee: Pharmacyclics, Inc.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Publication number: 20130040997Abstract: Provided are a novel pyridine carboxylic acid based compound used as a P2X1 and P2X3 receptor antagonist, a production method for the same and a composition comprising the same. The compound according to the present invention is a powerful antagonist of P2X1 and P2X3 receptors, and hence can be used as a drug for treating or preventing diseases involving neurological pain or chronic inflammatory diseases which are diseases caused by P2X1 and P2X3 receptor activity.Type: ApplicationFiled: December 20, 2010Publication date: February 14, 2013Applicant: GWANGJU INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Yong-Chul Kim, Kwan-Young Jung, Joong Heui Cho
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Publication number: 20130035351Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.Type: ApplicationFiled: August 3, 2011Publication date: February 7, 2013Applicant: SOUTHWEST RESEARCH INSTITUTEInventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
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Patent number: 8367666Abstract: The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1, R2, R3, R4, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.Type: GrantFiled: February 28, 2012Date of Patent: February 5, 2013Assignee: Shionogi & Co., Ltd.Inventors: Takashi Sasatani, Yoshiharu Hiramatsu, Susumu Mitsumori
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Publication number: 20130029965Abstract: A composition comprises a solid dispersion comprising a low-solubility drug and at least one polymer. In another aspect of the invention, a composition comprises a solid dispersion comprising a low-solubility drug and a stabilizing polymer. At least a major portion of the drug in the dispersion is amorphous. The composition also includes a concentration-enhancing polymer that increases the concentration of the drug in a use environment. The stabilizing polymer has a glass transition temperature that is greater than the glass transition temperature of the concentration-enhancing polymer at a relative humidity of 50%.Type: ApplicationFiled: September 11, 2012Publication date: January 31, 2013Applicant: BEND RESEARCH, INC.Inventors: Walter C. Babcock, Dwayne T. Friesen, James A. S. Nightingale, Ravi M. Shanker
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Publication number: 20130018040Abstract: Compositions and methods for the treatment of toxoplasmosis, caused by the infectious eukaryotic parasite Toxoplasma gondii (T. gondii) and for the treatment of cryptosporidiosis, caused by the infectious eukaryotic parasites Cryptosporidium parvum (C. parvum) and Cryptosporidium hominus (C. hominus) are described. In particular, the present disclosure is directed to compositions and methods for inhibiting either T. gondii calcium dependent protein kinases (TgCDPKs) or C. parvum and C. hominus calcium dependent protein kinases (CpCDPKs) using pyrazolopyrimidine and/or imidazo[1,5-a]pyrazine inhibitors, of the formula, wherein the variables X, Y, Z, L, R1, and R3 are defined herein.Type: ApplicationFiled: July 30, 2012Publication date: January 17, 2013Applicant: University of Washington through its Center for CommercializationInventors: Wesley C. VAN VOORHIS, Wilhelmus G.J. HOL, Eric T. LARSON, Dustin James MALY, Ethan MERRITT, Kayode K. OJO
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Publication number: 20130012531Abstract: The present invention is directed to methods of treating disorders of ocular angiogenesis or vascular leakage in a patient by administration of suitable inhibitors, including pazopanib or pharmaceutically acceptable salts or hydrates thereof.Type: ApplicationFiled: January 5, 2011Publication date: January 10, 2013Inventors: Andrew G King, Albert B. Suttle, Valeriu Damian-Iordache, Megan M Mclaughlin
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Publication number: 20130012550Abstract: The present invention also relates to biomarkers and the use of biomarkers for the prediction and prognosis of cancer as well as the use of biomarkers to monitor the efficacy of cancer treatment. Specifically, this invention relates to the use of HER-2, EGFR, VEGF, u-PA, p-PAI-1, and soluble forms thereof, as biomarkers for cancer, especially for subjects treated with sorafenib.Type: ApplicationFiled: September 13, 2012Publication date: January 10, 2013Applicant: BAYER HEALTHCARE LLCInventor: Scott Wilhelm
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Patent number: 8350043Abstract: Substituted pyridines, pyrimidines, pyrazines, pyridinones, pyrimidinones, pyrazinones and phenylacetamides useful in treating depression, stress and other disorders are disclosed. The compounds are of the formualae: Other embodiments are also disclosed.Type: GrantFiled: June 7, 2006Date of Patent: January 8, 2013Assignee: Pharmacopeia, Inc.Inventors: Jeffrey John Letourneau, Koc-Kan Ho, Michael J. Ohlmeyer, Patrick Jokiel, Christopher Mark Riviello
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Patent number: 8349832Abstract: The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed.Type: GrantFiled: September 2, 2010Date of Patent: January 8, 2013Assignees: Canthera Therapeutics, The Massachusetts General Hospital CorporationInventors: Michael Andrew Foley, Robert Gould, Peter Elliott, Anna Mandinova
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Publication number: 20120329836Abstract: Disclosed herein is {[5-(3-fluorophenyl)-3-hydroxypyridine-2-carbonyl]-amino}acetic acid and the ester and amide prodrugs thereof, that can stabilize hypoxia inducible factor-2 alpha (HIF-2?) and thereby provide a method for treating cancer. Further disclosed are compositions which comprise {[5-(3-fluorophenyl)-3-hydroxypyridine-2-carbonyl]-amino}acetic acid and/or a prodrug thereof which can be used to treat cancer.Type: ApplicationFiled: June 5, 2012Publication date: December 27, 2012Applicant: The Ohio State UniversityInventors: Clay B. Marsh, Timothy Darren Eubank, Julie Michelle Rhoda, Joseph H. Gardner, Robert Shalwitz
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Patent number: 8338457Abstract: The present invention provides methods and kits for the selective ablation of pain-sensing neurons. The methods comprise administration of a vanilloid receptor agonist to a ganglion in an amount that causes death of vanilloid receptor-bearing neurons. Accordingly, the present invention provides methods of controlling pain and inflammatory disorders that involve activation of vanilloid receptor-bearing neurons.Type: GrantFiled: May 7, 2010Date of Patent: December 25, 2012Assignee: The United States of America as represented by the Secretary of the Department of Human ServicesInventors: Michael J. Iadarola, Zoltan Olah, Laszlo Karai
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Patent number: 8334307Abstract: Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.Type: GrantFiled: October 7, 2011Date of Patent: December 18, 2012Assignee: Biotheryx Inc.Inventors: Frank Mercurio, Kyle W. H. Chan
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Publication number: 20120316147Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: June 1, 2012Publication date: December 13, 2012Inventors: Caterina Bissantz, Uwe Grether, Paul Hebeisen, Atsushi Kimbara, Qingping Liu, Matthias Nettekoven, Marco Prunotto, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch, Christoph Ullmer, Zhiwei Wang, Wulun Yang
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Patent number: 8324392Abstract: The present invention relates to a novel solid form of 4-[[(6-chloropyridin-3-yl)methyl](2,2-difluoroethyl)amino]furan-2(5H)-one, to processes for its preparation and to its use in agrochemical preparations.Type: GrantFiled: October 22, 2010Date of Patent: December 4, 2012Assignee: Bayer Cropscience AGInventors: Britta Olenik, Robert Velten, Peter Jeschke, Norbert Lui, Christian Funke, Wolfgang Wirth